Nabumetone

RELAFEN

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What it isNonacidic NSAID prodrug converted to an active cyclooxygenase inhibitor; osteoarthritis and rheumatoid arthritis.

Why this oneIts nonacidic prodrug design reduces direct gastric irritation, but not systemic gastrointestinal injury.

What limits itRenal injury, cardiovascular events, and GI bleeding still apply; it can also raise lithium levels.

FDA-approved for

arthritis (1991)

FDA label

Read the full label on DailyMed ↗

BOXED WARNING NSAID: increased risk of serious cardiovascular thrombotic events (MI, stroke) — contraindicated in CABG surgery; increased risk of serious GI bleeding, ulceration, and perforation.

FDA dosing	Population	Start	Target	Max
Osteoarthritis and rheumatoid arthritis	adult	1000 mg QD	1500–2000 mg/day (QD or BID)	2000 mg/day

Renal Undefined

Hepatic Undefined

Instructions

Take with or without food
Use lowest effective dose for shortest duration
May give as a single or twice-daily dose
Patients <50 kg may not require doses beyond 1000 mg/day

Contraindications

Setting of coronary artery bypass graft (CABG) surgery
Asthma, urticaria, or allergic-type reactions after aspirin or other NSAIDs

Cautions

Cardiovascular thrombotic events
GI bleeding/ulceration/perforation
Hepatotoxicity
Hypertension/edema/heart failure
Renal toxicity
Serious skin reactions (SJS, TEN, exfoliative dermatitis)
Anaphylactoid reactions

Adverse reactions

Diarrhea
Dyspepsia
Abdominal pain
Constipation
Flatulence
Nausea
Edema
Rash/pruritus
Tinnitus
Dizziness
Headache

Pregnancy Avoid at ~30 weeks gestation and later (premature ductus arteriosus closure); limit use 20–30 weeks (oligohydramnios risk)

Lactation Undefined

⚠ BOXED WARNINGS

Cardiovascular thrombotic events
Gastrointestinal bleeding, ulceration and perforation

Cost, est. cash$5–$150/month

Generic entry2000

Classes and tags

Clinical profile

Therapeutic safety burden2 / 4

Overdose danger3 / 4

Weight-gain liability0 / 4

Sedation liability0 / 4

QT / Torsades0 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk3 / 4

Legacy pregnancy categoryMultiple / indication-, trimester- or formulation-dependent

Defining liabilityGI bleeding, kidney injury, hypertension and fluid retention; many agents increase lithium concentrations.

Active metabolites

6-MNA

Mechanism of action: Nabumetone ballicule

Nabumetone ballicule: receptor binding, kinetics and half-life diagram

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Memory aids: mascots and interaction avatars

Nabumetone RELAFEN mascot mnemonic cartoon — **“Nabu’s boom tone is Relevant (or “Really late”)”**
“The N said... NSAID”

Box: minimal PK interactions

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